메뉴 건너뛰기




Volumn 33, Issue 8, 2008, Pages 691-699

The rise of second-generation non-nucleoside reverse transcriptase inhibitors: Etravirine, rilpivirine, UK-453061 and RDEA-806

Author keywords

[No Author keywords available]

Indexed keywords

ANTIVIRUS AGENT; DAPIVIRINE; DARUNAVIR; EFAVIRENZ; ENFUVIRTIDE; ETRAVIRINE; LOPINAVIR PLUS RITONAVIR; MIV 150; NEVIRAPINE; NUCLEOTIDYLTRANSFERASE INHIBITOR; PLACEBO; PROTEINASE INHIBITOR; RDEA 806; RILPIVIRINE; RITONAVIR; RNA DIRECTED DNA POLYMERASE INHIBITOR; UK 453061; UNCLASSIFIED DRUG;

EID: 59349111624     PISSN: 03778282     EISSN: None     Source Type: Journal    
DOI: 10.1358/dof.2008.033.08.1206423     Document Type: Review
Times cited : (6)

References (34)
  • 2
    • 0344149561 scopus 로고    scopus 로고
    • AIDS Clinical Trials Group 384 Team: Comparison of four-drug regimens and pairs of sequential three-drug regimens as initial therapy for HIV-1 infection
    • Shafer, R.W., Smeaton, L.M., Robbins, G.K. et al. AIDS Clinical Trials Group 384 Team: Comparison of four-drug regimens and pairs of sequential three-drug regimens as initial therapy for HIV-1 infection. N Engl J Med 2003, 49(24): 2304-15.
    • (2003) N Engl J Med , vol.49 , Issue.24 , pp. 2304-2315
    • Shafer, R.W.1    Smeaton, L.M.2    Robbins, G.K.3
  • 3
    • 33846029605 scopus 로고    scopus 로고
    • Long-term clinical and immunologic outcomes are similar in HIV-infected persons randomised to NNRTI vs. Pl vs. NNRT+Pl-based antiretroviral regimens as initial therapy: Results of NNRTI + the CPCRA 058 FIRST Study
    • Aug 13-18, Toronto, Abst TUAB0102
    • MacArthur, R.D., Novak, R.M., Pen, G. et al. Long-term clinical and immunologic outcomes are similar in HIV-infected persons randomised to NNRTI vs. Pl vs. NNRT+Pl-based antiretroviral regimens as initial therapy: Results of NNRTI + the CPCRA 058 FIRST Study. 16th Int AIDS Conf (Aug 13-18, Toronto) 2006, Abst TUAB0102.
    • (2006) 16th Int AIDS Conf
    • MacArthur, R.D.1    Novak, R.M.2    Pen, G.3
  • 5
    • 0037350147 scopus 로고    scopus 로고
    • Effects of HIV protease inhibitor therapy on lipid metabolism
    • Hui, D.Y. Effects of HIV protease inhibitor therapy on lipid metabolism. Prog Lipid Res 2003, 42(2): 81-92.
    • (2003) Prog Lipid Res , vol.42 , Issue.2 , pp. 81-92
    • Hui, D.Y.1
  • 6
    • 0033576816 scopus 로고    scopus 로고
    • Efavirenz plus zidovudine and lamivudine, efavirenz plus indinavir, and indinavir plus zidovudine and lamivudine in the treatment of HIV-1 infection in adults, Study 006 Team
    • Staszewski, S., Morales-Ramirez, J., Tashima, K.T. et al. Efavirenz plus zidovudine and lamivudine, efavirenz plus indinavir, and indinavir plus zidovudine and lamivudine in the treatment of HIV-1 infection in adults, Study 006 Team. N Engl J Med 1999, 341(25): 1865-73.
    • (1999) N Engl J Med , vol.341 , Issue.25 , pp. 1865-1873
    • Staszewski, S.1    Morales-Ramirez, J.2    Tashima, K.T.3
  • 7
    • 34547768212 scopus 로고    scopus 로고
    • Comparison of the effectiveness of initial combined antiretroviral therapy with nelfinavir or efavirenz at a university-based outpatient service in Brazil
    • Vanni, T., Morejón, K.M., Santana, R.C. et al. Comparison of the effectiveness of initial combined antiretroviral therapy with nelfinavir or efavirenz at a university-based outpatient service in Brazil. Braz J Med Biol Res 2007, 40(7): 963-9.
    • (2007) Braz J Med Biol Res , vol.40 , Issue.7 , pp. 963-969
    • Vanni, T.1    Morejón, K.M.2    Santana, R.C.3
  • 8
    • 0037016389 scopus 로고    scopus 로고
    • Virological suppression at 6 months is related to choice of initial regimen in antiretroviral-naïve patients: A cohort study
    • Matthews, G.V., Sabin, C.A., Mandalia, S. et al. Virological suppression at 6 months is related to choice of initial regimen in antiretroviral-naïve patients: A cohort study. AIDS 2002, 16(1): 53-61.
    • (2002) AIDS , vol.16 , Issue.1 , pp. 53-61
    • Matthews, G.V.1    Sabin, C.A.2    Mandalia, S.3
  • 9
    • 33845997533 scopus 로고    scopus 로고
    • A prospective, randomised, phase III trial of NRTI-, PI-, and NNRTI-sparing regimens for initial treatment of HIV-1 infection
    • Aug 13-18, Toronto, Abst THLB0204
    • Ridler, S.A., Haubrich, R., DiRienzo, G. et al. A prospective, randomised, phase III trial of NRTI-, PI-, and NNRTI-sparing regimens for initial treatment of HIV-1 infection, 16th Int AIDS Conf (Aug 13-18, Toronto) 2006, Abst THLB0204.
    • (2006) 16th Int AIDS Conf
    • Ridler, S.A.1    Haubrich, R.2    DiRienzo, G.3
  • 10
    • 0035037383 scopus 로고    scopus 로고
    • Genotypic correlates of phenotypic resistance to efavirenz in virus isolates from patients failing nonnucleoside reverse transcriptase inhibitor therapy
    • Bacheler, L., Jeffrey, S., Hanna, G. et al. Genotypic correlates of phenotypic resistance to efavirenz in virus isolates from patients failing nonnucleoside reverse transcriptase inhibitor therapy. J Virol 2001, 75(11): 4999-5008.
    • (2001) J Virol , vol.75 , Issue.11 , pp. 4999-5008
    • Bacheler, L.1    Jeffrey, S.2    Hanna, G.3
  • 11
    • 0034786988 scopus 로고    scopus 로고
    • Resistance profile and cross-resistance of HIV-1 among patients failing a non-nucleoside reverse transcriptase inhibitor-containing regimen
    • Delaugerre, C., Rohban, R., Simon, A. et al. Resistance profile and cross-resistance of HIV-1 among patients failing a non-nucleoside reverse transcriptase inhibitor-containing regimen. J Med Virol 2001, 65(3): 445-8.
    • (2001) J Med Virol , vol.65 , Issue.3 , pp. 445-448
    • Delaugerre, C.1    Rohban, R.2    Simon, A.3
  • 12
    • 0033840455 scopus 로고    scopus 로고
    • Human immunodeficiency virus type 1 mutations selected in patients failing efavirenz combination therapy
    • Bacheler, L.T., Anton, E.D., Kudish, P. et al. Human immunodeficiency virus type 1 mutations selected in patients failing efavirenz combination therapy. Antimicrob Agents Chemother 2000, 44(9): 2475-84.
    • (2000) Antimicrob Agents Chemother , vol.44 , Issue.9 , pp. 2475-2484
    • Bacheler, L.T.1    Anton, E.D.2    Kudish, P.3
  • 13
    • 20844451906 scopus 로고    scopus 로고
    • Emergence of drug-resistance HIV-1 after intrapartum administration of single-dose nevirapine is substantially underestimated
    • Johnson, J.A., Li, J.F., Morris, L. et al. Emergence of drug-resistance HIV-1 after intrapartum administration of single-dose nevirapine is substantially underestimated. J Infect Dis 2005, 192(1): 16-23.
    • (2005) J Infect Dis , vol.192 , Issue.1 , pp. 16-23
    • Johnson, J.A.1    Li, J.F.2    Morris, L.3
  • 14
  • 15
    • 0036782103 scopus 로고    scopus 로고
    • Inhibitor binding alters the directions of domain motions in HIV-1 reverse transcriptase
    • Temiz, N.A., Bahar, I. Inhibitor binding alters the directions of domain motions in HIV-1 reverse transcriptase. Proteins 2002, 49(1): 61-70.
    • (2002) Proteins , vol.49 , Issue.1 , pp. 61-70
    • Temiz, N.A.1    Bahar, I.2
  • 16
    • 22244487870 scopus 로고    scopus 로고
    • R165335-TMC125, a third generation non nucleoside reverse transcriptase inhibitor (NNRTI), inhibits 98% of more than 2000 recombinant HIV clinical isolates at 100 nM
    • Sept 17-20, Toronto, Abst F-1841
    • De Bethune, M.P., Hertogs, K., Azijn, H. et al. R165335-TMC125, a third generation non nucleoside reverse transcriptase inhibitor (NNRTI), inhibits 98% of more than 2000 recombinant HIV clinical isolates at 100 nM. 40th Intersci Conf Antimicrob Agents Chemother (ICAAC) (Sept 17-20, Toronto) 2000, Abst F-1841.
    • (2000) 40th Intersci Conf Antimicrob Agents Chemother (ICAAC)
    • De Bethune, M.P.1    Hertogs, K.2    Azijn, H.3
  • 17
    • 9644291579 scopus 로고    scopus 로고
    • TMC1225, a novel next-generation nonnucleoside reverse transcriptase inhibitor active against nonnucleoside reverse transcriptase inhibitor-resistant human immunodeficiency virus type 1
    • Andries, K., Azijn, H., Thielemans, T. et al. TMC1225, a novel next-generation nonnucleoside reverse transcriptase inhibitor active against nonnucleoside reverse transcriptase inhibitor-resistant human immunodeficiency virus type 1. Antimicrob Agents Chemother 2004, 48(12): 4680-6.
    • (2004) Antimicrob Agents Chemother , vol.48 , Issue.12 , pp. 4680-4686
    • Andries, K.1    Azijn, H.2    Thielemans, T.3
  • 18
    • 2342620790 scopus 로고    scopus 로고
    • Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 variants
    • Das, K., Clark, A.D., Lewi, P.J. et al. Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 variants. J Med Chem 2004, 47(10): 2550-60.
    • (2004) J Med Chem , vol.47 , Issue.10 , pp. 2550-2560
    • Das, K.1    Clark, A.D.2    Lewi, P.J.3
  • 20
    • 12144287763 scopus 로고    scopus 로고
    • An open-label assessment of TMC125 - A new, next-generation NNRTI, for 7 days in HIV-1 infected individuals with NNRT1 resistance
    • Gazzard, B., Pozniak, A., Rosenbaum, W. et al. An open-label assessment of TMC125 - A new, next-generation NNRTI, for 7 days in HIV-1 infected individuals with NNRT1 resistance. AIDS 2003, 17(18): F49-54.
    • (2003) AIDS , vol.17 , Issue.18
    • Gazzard, B.1    Pozniak, A.2    Rosenbaum, W.3
  • 21
    • 12144289848 scopus 로고    scopus 로고
    • A randomised, double-blind, placebo-controlled trial of TMC125 as 7-day monotherapy in antiretroviral naïve, HIV-1 infected subjects
    • Gruzdev, B., Rakhmanova, A., Doubovskaya, E. et al. A randomised, double-blind, placebo-controlled trial of TMC125 as 7-day monotherapy in antiretroviral naïve, HIV-1 infected subjects. AIDS 2003, 17(17): 2487-94.
    • (2003) AIDS , vol.17 , Issue.17 , pp. 2487-2494
    • Gruzdev, B.1    Rakhmanova, A.2    Doubovskaya, E.3
  • 22
    • 34347327010 scopus 로고    scopus 로고
    • Efficacy and safety of TMC125 (etravirine) in treatment-experienced HIV-1-infected patients in DUET-1: 24-Week results froma randomised, double-blind, placebo-controlled trial
    • Madruga, J., Cahn, P., Grinsztejn, B. et al. Efficacy and safety of TMC125 (etravirine) in treatment-experienced HIV-1-infected patients in DUET-1: 24-Week results froma randomised, double-blind, placebo-controlled trial. Lancet 2007, 370(9581): 29-38.
    • (2007) Lancet , vol.370 , Issue.9581 , pp. 29-38
    • Madruga, J.1    Cahn, P.2    Grinsztejn, B.3
  • 23
    • 34347354196 scopus 로고    scopus 로고
    • Efficacy and safety of TMC125 (etravirine) in treatment-experienced HIV-1-infected patients in DUET-2:24-Week results from a randomised, double-blind, placebo-controlled trial
    • Lazzarin, A., Campbell, T., Clotet, B. et al. Efficacy and safety of TMC125 (etravirine) in treatment-experienced HIV-1-infected patients in DUET-2:24-Week results from a randomised, double-blind, placebo-controlled trial. Lancet 2007, 370(9581): 39-48.
    • (2007) Lancet , vol.370 , Issue.9581 , pp. 39-48
    • Lazzarin, A.1    Campbell, T.2    Clotet, B.3
  • 24
    • 34147134958 scopus 로고    scopus 로고
    • Efficacy and safety of etravirine (TMC125) in patients with highly resistant HIV-1: Primary 24-week analysis
    • Nadler, J.P., Berger, D.S., Blick, G. et al. Efficacy and safety of etravirine (TMC125) in patients with highly resistant HIV-1: Primary 24-week analysis. AIDS 2007, 21(6): F1-10.
    • (2007) AIDS , vol.21 , Issue.6
    • Nadler, J.P.1    Berger, D.S.2    Blick, G.3
  • 25
    • 40549109383 scopus 로고    scopus 로고
    • Impact of NNRTI and NPTI resistance on the response to the regimen of TMC125 plus two NRT/s in study TMC125-C227
    • Nov 12-16, Glasgow, Abst PL5.6
    • Woodfall, B., Vingerhoets, J., Peeters, M. et al. Impact of NNRTI and NPTI resistance on the response to the regimen of TMC125 plus two NRT/s in study TMC125-C227. 8th Int Congr Drug Ther HIV Infect (Nov 12-16, Glasgow) 2006, Abst PL5.6.
    • (2006) 8th Int Congr Drug Ther HIV Infect
    • Woodfall, B.1    Vingerhoets, J.2    Peeters, M.3
  • 26
    • 20144366006 scopus 로고    scopus 로고
    • Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1
    • Guillemont, J., Pasquier, E., Palandjian, P. et al. Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1. J Med Chem 2005, 48(6): 2072-9.
    • (2005) J Med Chem , vol.48 , Issue.6 , pp. 2072-2079
    • Guillemont, J.1    Pasquier, E.2    Palandjian, P.3
  • 27
    • 20144372481 scopus 로고    scopus 로고
    • In search of a novel anti-HIV drug: Multidisciplinary coordination in the discovery of 4- 4-4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]- 2-pyrimidinyl]amino]benzonitrile (R278474, rilpivirine)
    • Janssen, P.A., Lewi, P.J., Arnold, E. et al. In search of a novel anti-HIV drug: Multidisciplinary coordination in the discovery of 4- 4-4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]- 2-pyrimidinyl]amino]benzonitrile (R278474, rilpivirine). J Med Chem 2005, 48(6): 1901-9.
    • (2005) J Med Chem , vol.48 , Issue.6 , pp. 1901-1909
    • Janssen, P.A.1    Lewi, P.J.2    Arnold, E.3
  • 28
    • 33748036988 scopus 로고    scopus 로고
    • Short-term antiviral activity of TMC278 - a novel NNRTI - in treatment-naive HIV-1-infected subjects
    • Goebel, F., Yakovlev, A., Pozniak, A.L. et al. Short-term antiviral activity of TMC278 - a novel NNRTI - in treatment-naive HIV-1-infected subjects. AIDS 2006, 20(13): 1721-6.
    • (2006) AIDS , vol.20 , Issue.13 , pp. 1721-1726
    • Goebel, F.1    Yakovlev, A.2    Pozniak, A.L.3
  • 29
    • 34249100738 scopus 로고    scopus 로고
    • 48-Week primary analysis of trial TMC278-C204: TMC278 demonstrates potent and sustained efficacy in ART-naive patients
    • Feb 25-28, Los Angeles, Abst 144LB. Available from
    • Pozniak, A., Morales-Ramirez, J., Mohapi, L. et al. 48-Week primary analysis of trial TMC278-C204: TMC278 demonstrates potent and sustained efficacy in ART-naive patients. 14th Conf Retroviruses Opportunistic Infect (CROI) (Feb 25-28, Los Angeles) 2007, Abst 144LB. Available from: http://www.retroconterence.org/2007/Abstracts/30659.htm
    • (2007) 14th Conf Retroviruses Opportunistic Infect (CROI)
    • Pozniak, A.1    Morales-Ramirez, J.2    Mohapi, L.3
  • 30
    • 46749084403 scopus 로고    scopus 로고
    • UK-453,061: A non-nucleoside reverse transcriptase inhibitor for the treatment of drug-resistant HIV infections
    • ICAAC, Sept 17-20, Chicago, Abst F1-945
    • Corbau, R., Allan, G., Burt, C. et al. UK-453,061: A non-nucleoside reverse transcriptase inhibitor for the treatment of drug-resistant HIV infections. 47th Intersci Cont Antimicrob Agents Chemother (ICAAC) (Sept 17-20, Chicago) 2007, Abst F1-945.
    • (2007) 47th Intersci Cont Antimicrob Agents Chemother
    • Corbau, R.1    Allan, G.2    Burt, C.3
  • 31
    • 59349086979 scopus 로고    scopus 로고
    • Safety, toleration and pharmacokinetics of single and multiple oral doses of UK 453,061, a novel NNRTi, in healthy male subjects
    • July 22-25, Sydney, Abst WEPEA 109
    • Davis, J., Jenkins, T., Asken, E., Stafford, H., Hackman, F., Weissgerber, G. Safety, toleration and pharmacokinetics of single and multiple oral doses of UK 453,061, a novel NNRTi, in healthy male subjects. 4th IAS Conf HIV Pathog Treat Prev (July 22-25, Sydney) 2007, Abst WEPEA 109.
    • (2007) 4th IAS Conf HIV Pathog Treat Prev
    • Davis, J.1    Jenkins, T.2    Asken, E.3    Stafford, H.4    Hackman, F.5    Weissgerber, G.6
  • 32
    • 35548937142 scopus 로고    scopus 로고
    • Shortterm monotherapy with UK-453,061, a novel NNRTI, reduces viral load in HIV infected patients
    • July 22-25, Sydney, Abst WESS202
    • Fätkenheuer, G., Staszewski, S., Plettenburg, A. et al. Shortterm monotherapy with UK-453,061, a novel NNRTI, reduces viral load in HIV infected patients. 4th IAS Conf HIV Pathog Treat Prev (July 22-25, Sydney) 2007, Abst WESS202.
    • (2007) 4th IAS Conf HIV Pathog Treat Prev
    • Fätkenheuer, G.1    Staszewski, S.2    Plettenburg, A.3
  • 33
    • 33746233238 scopus 로고    scopus 로고
    • Tri-substituted triazoles as potent non-nucleoside inhibitors of the HIV-1 reverse transcriptase
    • De La Rosa, M., Kim, H.W., Gunic, E. et al. Tri-substituted triazoles as potent non-nucleoside inhibitors of the HIV-1 reverse transcriptase. Bioorg Med Chem Lett 2006, 16(17): 4444-9.
    • (2006) Bioorg Med Chem Lett , vol.16 , Issue.17 , pp. 4444-4449
    • De La Rosa, M.1    Kim, H.W.2    Gunic, E.3


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.